A versatile stereocontrolled synthesis of 2-deoxyiminosugar C -glycosides and their evaluation as glycosidase inhibitors

Autor: Erwan Le Grognec, Carmen Ortiz Mellet, Alexandre Lumbroso, M. Isabel García-Moreno, Clément Berthonneau, Aurélien Planchat, Isabelle Beaudet, Jean-Paul Quintard

Publikováno v: Organic and Biomolecular Chemistry
Organic and Biomolecular Chemistry, Royal Society of Chemistry, 2021, 19 (5), pp.1083-1099. ⟨10.1039/d0ob02249g⟩

International audience; A highly enantioselective synthesis of (R,S) or (S,S)-2,6-disubstituted dehydropiperidines has been previously achieved through Sn/Li transmetalation of the corresponding stannylated dehydropiperidines or of their precursors.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::81f7d08bfb233a3d16e4bf48692fb1e3
https://hal.archives-ouvertes.fr/hal-03388809/document

Discovery of a series of selective and cell permeable beta-secretase (BACE1) inhibitors by fragment linking with the assistance of STD-NMR

Autor: Stefan F. Lichtenthaler, Shanshan Sun, Jian Huang, Chen Cheng, Wei-Shuo Fang, Ying-Hong Wang, Katrin Moschke, Shuang Yang, Deyang Sun, Tianqi Li

Publikováno v: Bioorganic chemistry 92, 103253 (2019). doi:10.1016/j.bioorg.2019.103253

Two β-secreatase (BACE1) inhibitors from natural products (cinnamic acid and flavone) were linked to furnish potent, cell permeable BACE1 inhibitors with noncompetitive mode of inhibition, with the assistance of saturated transfer difference (STD)-N

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::87706b9b7ac457762e8317189ae9c3c6

Unexpected active-site flexibility in the structure of human neutrophil elastase in complex with a new dihydropyrimidone inhibitor

Autor: Dietmar Schomburg, Axel Harrenga, Guido Hansen, Karsten Niefind, Heike Gielen-Haertwig, Peter Reinemer

Publikováno v: Journal of molecular biology 409, 681-691 (2011). doi:10.1016/j.jmb.2011.04.047

Human neutrophil elastase (HNE), a trypsin-type serine protease, is of pivotal importance in the onset and progression of chronic obstructive pulmonary disease (COPD). COPD encompasses a group of slowly progressive respiratory disorders and is a majo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0eb7018bf974b11b7282ecdcc17e4f94
https://bib-pubdb1.desy.de/record/94311

A zebrafish model of tauopathy allows in vivo imaging of neuronal cell death and drug evaluation

Autor: Ratan Bhat, Martin Distel, Astrid Sydow, Sven Hellberg, Bettina Schmid, Stefan von Berg, Eva-Maria Mandelkow, Christian Haass, Dominik Paquet, Reinhard W. Köster, Johanna Fälting

Publikováno v: The journal of clinical investigation 119(5), 1382-1395 (2009). doi:10.1172/JCI37537
Journal of Clinical Investigation; Vol 119
J. Clin. Invest. 119, 1382-1395 (2009)

Our aging society is confronted with a dramatic increase of patients suffering from tauopathies, which include Alzheimer disease and certain frontotemporal dementias. These disorders are characterized by typical neuropathological lesions including hy

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::114ca33e717b34d138f4036cc5ca11f9
https://pubmed.ncbi.nlm.nih.gov/19363289